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Method for preparing paeonol-ozagrel conjugate lipidosome through ethanol injection method

A technology of paeonol and conjugates, which is applied in the field of pharmaceutical preparation, can solve the problems of limitations, poor water solubility and fat solubility, etc., and achieve the effects of easy mastery, high drug loading and stable performance

Inactive Publication Date: 2017-07-14
上海海虹实业(集团)巢湖今辰药业有限公司
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  • Abstract
  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

However, the water solubility and fat solubility of this product are relatively poor, which greatly limits its clinical application.

Method used

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  • Method for preparing paeonol-ozagrel conjugate lipidosome through ethanol injection method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Measure 20 mL of phosphate buffer solution into a stoppered Erlenmeyer flask, put in a magnet, and stir on a collector heating stirrer with a rotation speed of 350 r / min and a set temperature of 35 °C. Precisely weigh 6 mg of ozagrel, 100 mg of soybean lecithin, and 5 mg of cholesterol into a stoppered Erlenmeyer flask, add 3 mL of absolute ethanol and sonicate for 4 minutes to dissolve them, inject the above drugs into the phosphate buffer slowly and uniformly with a 1 mL syringe, and continue After stirring for 2 hours, the final suspension was passed through a 0.80 μm microporous membrane to size the particles to obtain paeonol-ozagrel conjugate liposomes.

[0025] The drug loading and encapsulation efficiency of the paeonol-ozagrel conjugate liposome were determined to be 9.72% and 86.3%, respectively.

Embodiment 2

[0027] Measure 20 mL of phosphate buffer solution into a stoppered Erlenmeyer flask, put it into a magnet, and stir on a collector heating stirrer with a rotation speed of 300 r / min and a set temperature of 40 °C. Precisely weigh 9 mg of ozagrel, 150 mg of soybean lecithin, and 7.5 mg of cholesterol into a stoppered Erlenmeyer flask, add 3 mL of absolute ethanol and sonicate for 4 minutes to dissolve them, and inject the above drugs into the phosphate buffer slowly and uniformly with a 1 mL syringe. Stirring was continued for 2 hours, and the finally obtained suspension was sized through a 0.80 μm microporous membrane to obtain paeonol-ozagrel conjugate liposomes. The drug loading and encapsulation efficiency of the paeonol-ozagrel conjugate liposome were determined to be 9.92% and 87.4%, respectively.

Embodiment 3

[0029] Measure 20 mL of phosphate buffer solution into a stoppered Erlenmeyer flask, put it into a magnet, and stir on a collector heating stirrer with a rotation speed of 300 r / min and a set temperature of 40 °C. Precisely weigh 6 mg of ozagrel, 100 mg of soybean lecithin, and 10 mg of cholesterol into a stoppered Erlenmeyer flask, add 3 mL of absolute ethanol and sonicate for 4 minutes to dissolve them, inject the above drugs into the phosphate buffer slowly and uniformly with a 1 mL syringe, and continue After stirring for 2 hours, the final suspension was passed through a 0.80 μm microporous membrane to size the particles to obtain paeonol-ozagrel conjugate liposomes. The drug loading and encapsulation efficiency of paeonol-ozagrel conjugate liposomes were determined to be 9.62% and 84.6%, respectively.

[0030] Preparation Method 2 - Reverse Evaporation Method

[0031] Ratio of each component of paeonol-ozagrel conjugate liposome: paeonol-ozagrel conjugate: phospholipid ...

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Abstract

The invention discloses a method for preparing a paeonol-ozagrel conjugate lipidosome through an ethanol injection method. The paeonol-ozagrel conjugate lipidosome is prepared from a paeonol-ozagrel conjugate, a phospholipid material, cholesterol, an inorganic solvent and a buffer solution. The method comprises the steps of stirring a prescription dosage of phosphate buffer solution and setting the temperature to 40 DEG C; weighing a prescription dosage of paeonol-ozagrel conjugate, soybean lecithin and cholesterol into the absolute ethyl alcohol for ultrasonic treatment for 4min, slowly adding the drug to the phosphate buffer solution by using a 1mL injector at a constant speed, further stirring for two hours and granulating the finally obtained suspension through a 0.80micron microfiltration membrane to obtain the paeonol-ozagrel conjugate lipidosome. According to the method, the bioavailability and the stability of a paeonol-ozagrel conjugate are improved, thrill is reduced and the drug action time is prolonged.

Description

technical field [0001] The invention relates to a method for preparing paeonol-ozagrel conjugate liposome by an ethanol injection method, and belongs to the technical field of medicine preparation. Background technique [0002] Cardiovascular and cerebrovascular diseases are the main cause of death of the global population and seriously endanger human health. With the aging of the social population, the incidence is increasing day by day. Effective prevention and treatment of cardiovascular and cerebrovascular diseases are the focus of contemporary medical research [0003] Thromboembolism is one of the important factors leading to cardiovascular and cerebrovascular diseases. Thromboembolic disease is a pathological process in which various intrinsic and extrinsic factors lead to intravascular thrombus formation and embolism, resulting in impaired tissue and organ function. Thromboembolic diseases centered on coronary artery thrombosis and cerebral thrombosis have high morbi...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/55A61K31/12A61K31/4174A61P9/10A61P9/00A61P7/02
CPCA61K9/127A61K31/12A61K31/4174A61K2300/00
Inventor 彭灿金玉季凌涛陶俊钰刘修树
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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